1 - [(3, and 1 -[(3,5-difluorophenyI)methyl]-l,3-dihydro-2Himidazole-2-thione (SK&F 102048, SK&F 102055 and SK&F 102698, respectively) were synthesizyg in carbon-1 4 and tritium labeled forms Carbon-1 4 from potassium [ Clthiocyanate was incorporated into the imidazolethione ring of SK&F 102055 and
Carbon-14 labelled nitrogen heterocycles; the syntheses of three phosphodiesterase inhibitors
✍ Scribed by Kenneth W M Lawrie; Christine E A Novelli; David Saunders; William J Coates
- Publisher
- John Wiley and Sons
- Year
- 1995
- Tongue
- French
- Weight
- 362 KB
- Volume
- 36
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
The syntheses of three heterocyclic phosphodiesterase inhibitors are described from a common radiolabelled precursor, namely 2‐propoxybenzo[cyano‐^14^C]nitrile. Conversion of the nitrile to the corresponding methyl ketone or amidine allows elaboration of the heterocycles radiolabelled within the ring systems.
📜 SIMILAR VOLUMES
was a c c o m p l i s h e d b y t r a p p i n g f r o m 4 g a s chromatograph. The t e c h n i q u e of g a s -l i q u i d r a d i o c h r o m a t o g r a p h y i n a ct i v i t y d e t e r m i n a t i o n s i s d e s c r i b e d .
## Abstract A simple, high‐yielding synthesis of dibutyl[^14^C]formamide ([^14^C]DBF; **1**) from ^14^CO~2~ was developed (__Scheme 1__): reaction of LiBEt~3~H and ^14^CO~2~ followed by aqueous workup gave H^14^CO~2~H in high yield. Conversion of the [^14^C]formic acid to **1** was effected by a st